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A specific, photolabile and irreversible antagonist (L662,025) of the PAF-receptor.

Abstract：

:PAF (0.2 microM) induced maximal platelet aggregation in human PRP and [3H]-PAF (1-5 nM) binding to platelet membrane preparations had Kd value of 3.8 nM and Bmax of 200 fmoles/mg of protein. Without UV irradiation, a synthetic azido tetrahydrofuran derivative L662,025 was a reversible and competitive PAF-receptor antagonist with IC50 values of 5.6 +/- 0.3 microM (platelet aggregation) and 1.0 +/- 0.25 microM (receptor binding). Photolysis of L662,025 in the presence of PRP produced an irreversible inhibition of platelet aggregation and specific binding of [3H]-PAF (1 nM). L662,025 did not affect collagen- or ADP-induced human platelet aggregation before or after photolysis. It is a new probe that can be used to identify and characterize the PAF-receptor.

journal_name

Biochem Biophys Res Commun

journal_title

Biochemical and biophysical research communications

authors

Hussaini IM,Shen TY

doi

10.1016/0006-291x(89)91554-4

subject

Has Abstract

pub_date

1989-05-30 00:00:00

pages

23-30

issue

1

eissn

0006-291X

issn

1090-2104

pii

0006-291X(89)91554-4

journal_volume

161

pub_type

杂志文章

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